title: An update on the chemistry and medicinal chemistry of novel antimycobacterial compounds.
abstract: Tuberculosis (TB) is a serious public health issue, particularly in underdeveloped and developing countries. Furthermore the first-line anti-TB treatments were established over 40 years ago, multidrug-resistant Mycobacterium tuberculosis strains have been developed and the risk of coinfection with AIDS virus has highlighted this disease as a global emergency. The urgent need for more effective treatments against multidrug-resistant strains compatible with anti-AIDS drugs has prompted industries, governments and non-governmental agencies to pursue new drugs. In this study, we update the portfolio listed at Stop TB Partnership, present the biological activities as well as structure-activity relationship for these drugs and thoroughly discuss the synthetic methodologies used to produce these drugs.
authors.affiliation: Fundação Oswaldo Cruz (FIOCRUZ), Instituto de Tecnologia em Fármacos (Farmanguinhos), Departamento de Síntese de Fármacos, Laboratório de Síntese 1, Rua Sizenando Nabuco, 100, Manguinhos, CEP: 21041-250 - Rio de Janeiro, RJ - Brasil. boechat@far.fiocruz.br.
authors.forename: Frederico Silva Castelo
authors.initials: FS
authors.lastname: Branco
authors.forename: Angelo C
authors.initials: AC
authors.lastname: Pinto
authors.forename: Núbia
authors.initials: N
authors.lastname: Boechat
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D064687:Diarylquinolines / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D009593:Nitroimidazoles / Q000737:chemistry / Q000494:pharmacology; D010080:Oxazoles / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy
chemical_list: D019380:Anti-HIV Agents; D000995:Antitubercular Agents; D064687:Diarylquinolines; D009593:Nitroimidazoles; C516022:OPC-67683; D010080:Oxazoles; C493870:bedaquiline